Acetonitrile → 2-(1-(Methylsulfonyl)-1,2,3,6-tetrahydropyridin-4-yl)-5-((1-((1-(trifluoromethyl)cyclopropyl)methyl)piperidin-4-yl)methoxy)pyridine

Participants

Reaction Conditions

Reaction Steps

To Preparation 6 (206 mg, 0.586 mmol), potassium carbonate (243 mg, 1.76 mmol) and acetonitrile (2.93 mL, 56 mmol) in a microwave vial is added (1-(trifluoromethyl)cyclopropyl)methyl methanesulfonate (256 mg, 1.17 mmol). The microwave vial is sealed and heated at 140° C. for 2 h then 150° C. for 30 min in the Biotage microwave. The reaction is diluted with dichloromethane and water. The organic layer is separated and washed with brine, dried over sodium sulfate, filtered, and concentrated in vacuo. The residue is triturated with diethylether and the title product is collected via vacuum filtration to obtain 0.181 g of the title compound. MS (m/z) 474 (M+1).

Provenance & Evidence